Fawcett Caitlin, Tickle Joseph R, Coles Charlotte H
Large Molecule Discovery, GSK, GSK Medicines Research Centre, Stevenage, UK.
Department of Pure and Applied Chemistry, University of Strathclyde, Glasgow, UK.
MAbs. 2024 Jan-Dec;16(1):2311992. doi: 10.1080/19420862.2024.2311992. Epub 2024 Feb 21.
A major driver for the recent investment surge in bispecific antibody (bsAb) platforms and products is the multitude of distinct mechanisms of action that bsAbs offer compared to a combination of two monoclonal antibodies. Four bsAb products were granted first regulatory approvals in the US or EU during 2023 and the biopharmaceutical industry pipeline is brimming with bsAb candidates across a broad range of therapeutic applications. In previously reported bsAb discovery campaigns, following a hypothesis-based choice of two specific target proteins, selections and screening activities have often been performed in mono-specific formats. The conversion to bispecific modalities has usually been positioned toward the end of the discovery process and has involved small numbers of lead molecules, largely due to challenges in expressing, purifying, and analyzing large numbers of bsAbs. In this review, we discuss emerging strategies to facilitate the production of expanded bsAb panels, focusing particularly upon combinatorial methods to generate bsAb matrices. Such technologies will enable screening in. bispecific formats at earlier stages of discovery campaigns, not only widening the accessible protein space to maximize chances of success, but also advancing empirical bi-target validation activities to assess initial target selection hypotheses.
双特异性抗体(bsAb)平台及产品近期投资激增的一个主要驱动因素是,与两种单克隆抗体组合相比,bsAb具有多种不同的作用机制。2023年期间,有四种bsAb产品在美国或欧盟首次获得监管批准,生物制药行业的研发管线中充满了针对广泛治疗应用的bsAb候选药物。在先前报道的bsAb发现活动中,在基于假设选择两种特定靶蛋白之后,筛选活动通常以单特异性形式进行。向双特异性形式的转化通常定位在发现过程的末尾,并且涉及的先导分子数量较少,这主要是由于表达、纯化和分析大量bsAb存在挑战。在本综述中,我们讨论了促进生产扩展的bsAb库的新兴策略,特别关注生成bsAb矩阵的组合方法。此类技术将能够在发现活动的早期阶段以双特异性形式进行筛选,这不仅会扩大可探索的蛋白质空间以最大化成功机会,还会推进经验性双靶点验证活动,以评估初始靶点选择假设。